C07F9/572

PHOSPHATE DERIVATIVES OF RORGAMMA MODULATORS AND USES THEREOF

The present invention relates to phosphate derivatives of formula (I), and their therapeutic uses, preferably for treating a respiratory disease. The present invention further relates to pharmaceutical compositions and devices comprising such compounds.

NOVEL PRODRUGS AND CONJUGATES OF DIMETHYLTRYPTAMINE
20230041584 · 2023-02-09 ·

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.8, R.sub.9, X, Y, Z, W, and m are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.

##STR00001##

SALTS OF PRODRUGS OF PIPERAZINE AND SUBSTITUTED PIPERIDINE ANTIVIRAL AGENTS

This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection.

##STR00001## wherein: X is C or N with the proviso that when X is N, R.sup.1 does not exist; W is C or N with the proviso that when W is N, R.sup.2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of

##STR00002##

Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I.

##STR00003## wherein: L and M are independently selected from the group consisting of C.sub.1-C.sub.6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

PROCESS FOR THE PREPARATION OF ACYLPHOSPHANES
20180002357 · 2018-01-04 · ·

The present invention provides a process for the preparation of mono- and bisacylphosphanes based on formula (I):

##STR00001##

as well as for their corresponding oxides or sulfides. The present invention further relates to photoinitiators obtainable by said process.

PROCESS FOR THE PREPARATION OF ACYLPHOSPHANES
20180002357 · 2018-01-04 · ·

The present invention provides a process for the preparation of mono- and bisacylphosphanes based on formula (I):

##STR00001##

as well as for their corresponding oxides or sulfides. The present invention further relates to photoinitiators obtainable by said process.

Protease inhibitors for treatment of coronavirus infections

Provided herein are compounds of Formula (I), their pharmaceutically acceptable salts, and their pharmaceutical compositions: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4, R.sup.5, and A are defined in the present disclosure. The compounds are potent inhibitors of the main protease (M.sup.pro) of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2), and they are useful in treating or preventing COVID-19 in a subject.

Phenylpyrrolidinone formyl peptide 2 receptor agonists

The disclosure relates to compounds of Formulae (I)-(IX), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases. ##STR00001##

Phenylpyrrolidinone formyl peptide 2 receptor agonists

The disclosure relates to compounds of Formulae (I)-(IX), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases. ##STR00001##

CHIRAL SYNTHESIS OF A TERTIARY ALCOHOL

Disclosed herein are methods for preparing tertiary alcohols from an optionally substituted phenyl ketone or an optionally substituted pyridinyl ketone that includes the use of a chiral ligand and boron trifluoride diethyl etherate. Tertiary alcohols can be used to prepare synthetic versions of natural products and/or pharmaceuticals.

CHIRAL SYNTHESIS OF A TERTIARY ALCOHOL

Disclosed herein are methods for preparing tertiary alcohols from an optionally substituted phenyl ketone or an optionally substituted pyridinyl ketone that includes the use of a chiral ligand and boron trifluoride diethyl etherate. Tertiary alcohols can be used to prepare synthetic versions of natural products and/or pharmaceuticals.